چکیده (انگلیسی):

The aim of this study was to evaluate the effect of increasing
epinephrine load on the characteristics of fast-disintegrating
sublingual tablets for the potential emergency treatment of
anaphylaxis. Four tablet formulations, A, B, C, and D, containing
0%, 6%, 12%, and 24% of epinephrine bitartrate,
respectively, and microcrystalline cellulose:low-substituted
hydroxypropyl cellulose (9:1), were prepared by direct compression,
at a range of compression forces. Tablet weight
variation, content uniformity, hardness, disintegration time,
wetting time, and friability were measured for each formulation
at each compression force. All 4 tablet formulations
at each compression force were within the United States
Pharmacopeia (USP) limits for weight variation and content
uniformity. A linear increase in compression force
resulted in an exponential increase in hardness for all formulations,
a linear increase in disintegration and wetting
times of A, and an exponential increase in disintegration
and wetting times of B, C, and D. At a mean ± SD hardness
of ≥2.3 ± 0.2 kg, all tablet formulations passed the
USP friability test. At a mean ± SD hardness of ≤3.1 ±
0.2 kg, all tablet formulations resulted in disintegration and
wetting times of G10 seconds and G30 seconds, respectively.
Tablets with drug loads from 0% to 24% epinephrine
can be formulated with hardness, disintegration times,
and wetting times suitable for sublingual administration.